Synthesis, biological evaluation, and molecular docking studies of novel 1,2,3-triazole derivatives as potent anti-inflammatory agents

被引:28
作者
Kumar, A. Kishore [1 ]
Sunitha, V. [1 ]
Shankar, B. [1 ]
Ramesh, M. [1 ]
Krishna, T. Murali [2 ]
Jalapathi, P. [1 ]
机构
[1] Osmania Univ, Dept Chem, Univ Coll Sci, Hyderabad 500004, Andhra Pradesh, India
[2] Chaitanya Postgrad Coll Autonomous, Dept Biotechnol, Warangal 506001, Andhra Pradesh, India
关键词
1,2,3-triazoles; click chemistry; anti-inflammatory; docking; CLICK CHEMISTRY; CYCLOOXYGENASE; ASPIRIN; DRUGS; INHIBITION; AZIDES;
D O I
10.1134/S1070363216050297
中图分类号
O6 [化学];
学科分类号
070301 [无机化学];
摘要
In the present study, a novel series of 1,2,3-triazole derivatives have been synthesized using click chemistry approach. The structures were confirmed by spectroscopic methods. The products were screened for their in vivo anti-inflammatory activity. The tested compounds 6a, 6f, 6g, 6i, 6j, 6n, and 6p, demonstrated potent anti-inflammatory activity compared to the reference drug ibuprofen. Molecular docking studies of these 1,2,3-triazole derivatives into the active site of human cyclooxygenase-2 (COX-2) (PDB code 4PH9) demonstrated good affinity for the enzyme and suggested binding properties similar to ibuprofen.
引用
收藏
页码:1154 / 1162
页数:9
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